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. 2005 Sep 15;15(18):4029-32.
doi: 10.1016/j.bmcl.2005.06.028.

Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists

Xiaojun Han  1 , Sokhom S Pin, Kevin Burris, Lawrence K Fung, Stella Huang, Matthew T Taber, Jie Zhang, Gene M Dubowchik
Affiliations

Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists

Xiaojun Han et al. Bioorg Med Chem Lett. .

Abstract

8-Aryl-1,3a,8-triaza-cyclopenta[a]indenes represent a novel series of high binding affinity corticotropin-releasing factor 1 receptor antagonists. Here, we report their synthesis, SAR, and pharmacokinetic properties of compound 8e (K(i) = 23 nM).

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